Apitope Announces Publication of Graves’ Disease Data in International Peer-Reviewed Journal, Endocrinology

Apitope Announces Publication of Graves’ Disease Data in International Peer-Reviewed Journal, Endocrinology

HASSELT, Belgium, and CHEPSTOW, UK, 14 August 2018 – Apitope, a clinical stage biotech company developing potential first-in-class antigen-specific immunotherapies targeting autoimmune diseases, today announces publication of its pre-clinical Graves’ disease data in Endocrinology, one of the leading peer-reviewed endocrinology medical journals.

The publication entitled: Immunotherapy with apitopes® blocks the immune response to thyroid stimulating hormone receptor in HLA-DR transgenic mice , reports the results from a series of studies to identify peptides that can be used to treat the abnormal immune response to TSHR (thyroid stimulating hormone receptor) in Graves’ disease patients and can be found here.

The study showed that a mixture of two immunodominant apitopes® was sufficient to suppress both the abnormal T cell and antibody response to TSHR in HLA-DR transgenic mice. Tolerance induction was not disrupted by current drug treatments for Graves’ disease. The paper concluded antigen-specific immunotherapy with apitopes® from TSHR is a suitable approach for the treatment of Graves’ disease.

Dr Keith Martin, CEO of Apitope, said: “It is very encouraging to have these findings by our talented team of scientists published in Endocrinology, one of the most highly-regarded journals in the field. The data shows that immunotherapy with apitopes® is a suitable approach to be investigated for the treatment of Graves’ disease and demonstrate the potential to be the first disease-modifying treatment, as well as the first innovative therapy for Graves’ disease in more than 60 years.”

Prof David Wraith, CSO of Apitope, said: “I am excited to see these data published because it provides further evidence of the broad applicability of the Apitope platform to identify peptide apitopes® to treat a wide range of autoimmune diseases. The initial clinical data announced earlier this year confirmed the potential for the apitopes® reported in this publication to make a significant impact in the treatment of Graves’ disease.”

Apitope announces positive results with novel treatment for Graves’ disease

Phase I data show early efficacy in the majority of patients and a very favourable safety profile

HASSELT, Belgium, and CHEPSTOW, UK, 16 April 2018 – Apitope, a clinical stage biotech company developing potential first-in-class antigen-specific immunotherapies targeting autoimmune diseases (including multiple sclerosis (MS), Graves’ disease and uveitis), today announced positive results from the Phase I first in man clinical trial of its product candidate, ATX-GD-59, in development for the treatment of Graves’ disease.

Graves’ disease is one of the most common autoimmune diseases with approximately 10 million patients across Europe and the US and yet there have been no innovative treatments in more than 60 years. With Graves’ disease, the immune system mistakenly attacks the thyroid gland and causes it to become overactive. Symptoms can include an enlargement of the thyroid gland, swelling of the neck, localised abnormalities of skin, tremors, heat intolerance and sweating, significant weight loss, osteoporosis, atrial fibrillation and ocular changes in patients. Each year 20-30 out of every 100,000 people are newly diagnosed with Graves’ disease. The ratio of women versus men diagnosed with Graves’ disease is 6:1 and around 2% of all women will develop Graves’ disease during their lifetime.

Dr Simon Pearce, Professor of Endocrinology, Newcastle University, and Chief Investigator for the trial commenting on the results said: “It is very exciting to see these promising Phase I results where ATX-GD-59 has shown both an encouraging safety and tolerability profile as well as efficacy. With current first-line treatments having a high failure rate, and the second-line treatments being either invasive surgery or radioiodine, ATX-GD-59 demonstrates the potential to address the high medical need for a new, safe and effective treatment for the neglected field of those suffering from Graves’ disease.”

The Phase I clinical study met the primary endpoint to assess the safety and tolerability of ATX-GD-59 in 12 patients with Graves’ disease. The majority of the per protocol subjects were either euthyroid, the clinical objective of therapy, or close to being euthyroid by the end of treatment; the effect was maintained during the 3 months follow up off therapy. Importantly, TSHR antibody levels were also reduced with close correlations between percentage decreases in antibody and thyroid hormone levels in line with the mechanism of action.

Dr Keith Martin, Chief Executive Officer of Apitope, commented: “We’re highly encouraged by these data as they provide further evidence that our Apitope® platform identifies safe and effective treatments for autoimmune diseases. These findings are important for Graves’ disease patients in providing a potential new treatment paradigm aimed at the cause of the disease not just the symptoms. We will continue to progress the development of ATX-GD-59 as a treatment for Graves’ disease and are currently preparing to initiate a Phase II study in the first quarter of 2019.”

The investigational product was administered intradermally (ID) every two weeks over a period of 18 weeks in male and female patients that were not otherwise being treated with anti-thyroid therapy. Following a titration period of 25, 50, 100, 400 and 800 μg in the initial eight weeks of treatment, a dose of 800 μg was administered fortnightly for an additional 10 weeks, comparable to the regime followed in the successful ATX-MS-1467 multiple sclerosis (MS) trials.

Apitope Treatment Approach Published in Nature Communications – Scientists discover how to ‘switch off’ autoimmune diseases

Diepenbeek, Belgium – 4th September 2014 – Apitope, the drug discovery and development company focused on disease-modifying treatments for patients with autoimmune and allergic diseases, announced today that Bristol University research led by Apitope Founder and CSO, Prof David Wraith, on its treatment approach to autoimmune diseases, such as Multiple Sclerosis (MS), has been published in Nature Communications.

The researchers at the University of Bristol reported an important breakthrough in the fight against debilitating autoimmune diseases such as Multiple Sclerosis. Rather than the body’s immune system destroying its own tissue by mistake, researchers have discovered how cells convert from being aggressive to actually protecting against disease. It’s hoped this latest insight will lead to the widespread use of antigen-specific immunotherapy as a treatment for many autoimmune disorders, including Multiple Sclerosis (MS), Factor VIII intolerance in haemophiliacs, Graves’ disease (hyperthyroidism) and uveitis, conditions for which Apitope is developing important new therapies.

Commenting on the research, Dr. Keith Martin, CEO said: “Multiple Sclerosis affects around 100,000 people in the UK and 2.5 million people worldwide. This is an important breakthrough in our fight against debilitating autoimmune diseases by providing further important information on how to stop cells attacking healthy body tissue. This research further reinforces Apitope’s treatment approach, which has already successfully completed two clinical trials in MS patients with MRI data showing a significant decrease in new lesions, and has the potential to improve the lives of millions of people worldwide. Importantly, we are now taking this approach into other serious autoimmune conditions as well as MS.

The reported study, funded by the Wellcome Trust, is published in Nature Communications. The article entitled “Sequential transcriptional changes dictate safe and effective antigen-specific immunotherapy” that describes how researchers have managed to “switch off” autoimmune disease as a breakthrough for Multiple Sclerosis (MS) treatment, can be viewed here:http://www.nature.com/ncomms/2014/140903/ncomms5741/full/ncomms5741.html

Apitope Progresses Graves’ Disease Treatment Initiates Preclinical Development of Peptide Therapy

Diepenbeek, Belgium – 21st June 2014 – Apitope, the drug discovery and development company focused on disease-modifying treatments for patients with autoimmune and allergic diseases, announced today that it has started preclinical development of its novel peptide therapy ATX-GD-459 for the treatment of Graves’ disease.

Apitope, through its innovative discovery platform, has selected three peptides in ATX-GD-459 that have the potential to treat and prevent the production of stimulating antibodies against TSHR (thyroid stimulating hormone receptor) that lead to Graves’ disease.

Graves’ disease is an autoimmune disorder that impacts over 7.5 Million people worldwide. Patients with Graves’ disease typically develop goitre and serious medical issues such as increased heart rate, muscle weakness, disturbed sleep, and irritability. It affects multiple systems of the body, including the skin, heart, circulation and nervous system with potential long term morbidity. Some 30-50% of Graves’ disease patients develop the medically challenging Graves’ orbitopathy characterised by bulging eyes (proptosis), while 3-5% of such patients suffer from a sight- threatening form of Graves’ orbitopathy.

Graves’ disease is linked to the thyroid gland and the overproduction of the thyroid hormones thyroxine (T4) and triiodothyronine (T3). The overproduction of thyroid hormones is caused by auto-reactive T and B lymphocytes targeting the primary auto-antigen, TSHR. This activation of the thyroid cells through the auto-antibodies results in the typical Graves’ disease hyperthyroidism and respective symptoms.

Dr. Keith Martin, CEO said “Apitope is developing innovative products based on therapeutic peptides to treat a range of life-threatening autoimmune and allergic diseases, including rare conditions. We are delighted to progress the development of these innovative peptides which have the potential to help Graves’ disease patients. We now have seven programmes in clinical, and preclinical development and discovery as we continue to maximise the potential of our innovative discovery platform.”

The development of ATX-GD-459 is part of the DAVIAD project (www.daviad.eu) co-financed by the European Commission in the 7th Framework Programme, FP7-HEALTH-2013-INNOVATION-1, 602779. The DAVIAD consortium is comprised of Apitope as coordinator, GlaxoSmithKline Biologicals SA, Quintiles Benefit and KWS Biotest Limited.

Prof David Wraith, CSO and Founder of Apitope, added, “Bringing this latest product through into preclinical development is another important milestone event for Apitope and provides further evidence that our discovery platform can generate new potentially life changing therapies for development and validates further the scientific basis of our approach.”